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公开(公告)号：KR1019960011370B1
公开(公告)日：1996-08-22
申请号：KR1019910025885
申请日：1991-12-31
Applicant: 한국화학연구원
IPC: C07D209/12
CPC classification number: C07D221/20 , C07D209/54 , Y02P20/55
Abstract: Spiroalkylamine derivatives and their salts have a general formula (I), wherein R1 is hydrogen, substituted or unsubstituted C1-C20 alkyl, substituted or unsubstituted benzyl, formyl, substituted or unsubstituted C1-C5 alkylcarbonyl, substituted or unsubstituted benzoyl, substituted or unsubstituted C1-C5 alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, substituted or unsubstituted C1-C5 alkylsulfonyl, or substituted or unsubstituted benzenesulfonyl; R2 is hydrogen or methyl substituted at the position of 4 or 6; R3 is hydroxy, hydroxymethyl, carboxy, C1-C4 alkoxy, C2-C5 alkoxymethyl, C2-C5 acyloxy, C3-C6 acyloxymethyl, methanesulfonyloxy, methanesulfonyloxymethyl, p-toluenesulfonyloxy, p-toluenesulfonyloxymethyl, cyanato, C2-C6 alkoxycarbonyl, azidocarbonyl, C1-C8 alkyl, C1-C5 alkoxycarbonyl, aminocarbonyl substituted or unsubstituted benzyl or -(CH2)m-NR4R5, where m is 0 or 1; R4 is hydrogen, C1-C4 alkanoyl or benzoyl; and R5 is hydrogen, C1-C4 -alkyl, nitrogen protective group degradable in a living body, n is 1 or 2, diastereomers may be (1,3)-R,S, (1,3)-R,R, (1,3)-S,S or (1,3)-S,R.
Abstract translation: 螺烷基胺衍生物及其盐具有通式（I），其中R1是氢，取代或未取代的C1-C20烷基，取代或未取代的苄基，甲酰基，取代或未取代的C1-C5烷基羰基，取代或未取代的苯甲酰基，取代或未取代的C1 C 5烷氧基羰基，取代或未取代的苄氧基羰基，取代或未取代的C 1 -C 5烷基磺酰基，或取代或未取代的苯磺酰基; R2为4或6位的氢或甲基取代; R3是羟基，羟甲基，羧基，C1-C4烷氧基，C2-C5烷氧基甲基，C2-C5酰氧基，C3-C6酰氧基甲基，甲磺酰氧基，甲磺酰氧基甲基，对甲苯磺酰氧基，对甲苯磺酰氧基甲基，氰基，C2-C6烷氧羰基，叠氮羰基，C1 C 1-8烷基，C 1 -C 5烷氧基羰基，氨基羰基取代或未取代的苄基或 - （CH 2）m -NR 4 R 5，其中m为0或1; R4是氢，C1-C4烷酰基或苯甲酰基; R5为氢，C1-C4烷基，可在生物体中降解的氮保护基，n为1或2，非对映异构体可为（1,3）-R，S，（1,3）-R，R（（ 1,3）-S，S或（1,3）-S，R。
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公开(公告)号：KR1019940002955B1
公开(公告)日：1994-04-09
申请号：KR1019910006363
申请日：1991-04-20
Applicant: 한국화학연구원
IPC: C07D487/04
Abstract: The quinolone cpd. or its salts of formula (I) are prepd. by heating and reacting the cpd. (II) with the cpd. (III) or (IIIa) in presence of the base. In the formulas, R1 is opt. substd. C1-7 lower alkyl, opt. substd. C3-7 cycloalkyl, opt. substd. lower alkenyl, opt. substd. phenyl; R2 is H, protecting gp. of carboxyl gp. or pharmaceutically usuable metalic or organic cation; R3 is H or C1-4 lower alkyl, C2-4 hydroxy alkyl, C3-7 cycloalkyl or biodegradable N-protecting gp.; X is Cl or Br; Z is methyl; n is 1-3; n is 1 or 2; A is Cl or Br; L is halogen, ethane sulfonyl or paratoluene sulfonyl. The compound is antibacterial.
Abstract translation: 喹诺酮cpd 或其式（I）的盐是制备的。 通过加热和反应cpd。 （II）与cpd。 （III）或（IIIa）。 在公式中，R1是opt。 substd。 C1-7低级烷基，选择。 substd。 C3-7环烷基， substd。 低级链烯基 substd。 苯基; R2是H，保护gp。 的羧基gp。 或药学上可用的金属或有机阳离子; R3是H或C1-4低级烷基，C2-4羟基烷基，C3-7环烷基或可生物降解的N-保护性gp。 X是Cl或Br; Z是甲基; n为1-3; n为1或2; A是Cl或Br; L是卤素，乙磺酰基或对甲苯磺酰基。 该化合物是抗菌的。
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公开(公告)号：KR1019930006164B1
公开(公告)日：1993-07-08
申请号：KR1019910001726
申请日：1991-02-01
Applicant: 한국화학연구원
IPC: C07D487/04
Abstract: Quninolone derivs. of formula (I) and their salts are new. In (I), R1=H, carboxyl protecting gp., Na or K; R2=C1-6 alkyl, halogenated alkyl, alkenyl, C3-6 cycloalkyl, (halogenated) phenyl or X-O(or S)-CH2CH(CH3)-N-; Z=H, halogen or amino; R3=Cl, Br or F; X=N or C-Y; Y=H, F, Cl, Br or CH3; R4= cycloalkyl, hydroxy, hydroxyalkyl, amino or biode-gradable nitrogen protecting gp.; m = 1- 3; n = 1-2. Also claimed is the prepen. of (I) which comprises a condensation reaction of a cpd. of formula (II) with a cpd. of formula (III) in a solvent in the presence of a base at 15-200 deg.C. The cpds. (I) have a good antibacterial activity.
Abstract translation: Quninolone衍生物。 的式（I）及其盐是新的。 在（I）中，R 1 = H，羧基保护基，Na或K; R 2 = C 1-6烷基，卤代烷基，烯基，C 3-6环烷基，（卤代）苯基或X-O（或S）-CH 2 CH（CH 3） Z = H，卤素或氨基; R3 = Cl，Br或F; X = N或C-Y; Y = H，F，Cl，Br或CH 3; R4 =环烷基，羟基，羟基烷基，氨基或生物降解氮保护gp。 m = 1- 3; n = 1-2。 还声称是prepen。 的（I），其包含cpd的缩合反应。 的式（II）与cpd。 式（III）的化合物在溶剂中，在碱存在下，在15-200℃。 cpds。 （I）具有良好的抗菌活性。
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Patent Agency Ranking
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公开(公告)号：KR1019940002953B1
公开(公告)日：1994-04-09
申请号：KR1019910006267
申请日：1991-04-19
Applicant: 한국화학연구원
IPC: C07D401/14
Abstract: An organic acid salt of quinolone carboxylic acid or its hydrate, of formula (I) is new. The cpd. (I) is prepd. by adding the org. acid to the quinolone carboxylic acid dervs. cpd. of formula (II) in the solvent comprising C1-4 haloalkane, C1-3 lower alcohol or their mixt. or water. In the formulas, X is N or C-Y, Y= H, F or CH3; R1 is C1-6 alkyl, hydroxy alkyl, vinyl, or C3-6 cycloalkyl or F-substd. phenyl; R2 is H, CH3, ethyl or 2-hydroxy ethyl; m is 1-3; n is 1-2; Z is H, amino, halogen or CH3; A is lactic acid, ascorbic acid, maleic acid, malonic acid, glutamic acid, cytric acid, fumaric acid, paratoluene sulfonic acid, acetic acid, propionic acid, or tartaric acid.
Abstract translation: 式（I）的喹诺酮羧酸或其水合物的有机酸盐是新的。 cpd。 （I）是prepd。 通过添加组织。 酸对喹诺酮羧酸衍生物。 CPD。 （II）的溶剂在包含C 1-4卤代烷烃，C 1-3低级醇或其混合物的溶剂中。 或水。 在该式中，X是N或C-Y，Y = H，F或CH 3; R 1是C 1-6烷基，羟基烷基，乙烯基或C 3-6环烷基或F-杂原子。 苯基; R2是H，CH3，乙基或2-羟基乙基; m为1-3; n为1-2; Z是H，氨基，卤素或CH 3; A是乳酸，抗坏血酸，马来酸，丙二酸，谷氨酸，麦芽酸，富马酸，对甲苯磺酸，乙酸，丙酸或酒石酸。
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公开(公告)号：KR1019930008224B1
公开(公告)日：1993-08-27
申请号：KR1019910003933
申请日：1991-03-12
Applicant: 한국화학연구원
IPC: C07D207/20
CPC classification number: Y02P20/55
Abstract: Pyrolidine derivs. of formula (I) and their acid salts are prepd. In (I), R1=H or lower alkyl (C1-4), R2, R3=H, lower alkyl (C1-3), cycloalkyl, or -OH, and n = 1 or 2. The cpds. of formula (II) are reacted with triethyl phosphonoacetate or ethyl bromoacetate triphenyl phosphonic acid in the presence of strong base to give cpds. of formula (III) which have exo double bond. In cpds. (III), nitrogen protective group is subtd. with ethoxy carbonyl group and then ester is reduced to give alcoholic cpds. These cpds. are converted to methane sulfonyl derivs, and NH(R2R3) is subtd. to give cpds. (VII). Cpds. (VII) are hydrolyzed to give cpds. (I). Cpds. (I) are useful as the intermediates in the prepn. of quinolone or cephalosphorin antibiotics.
Abstract translation: 吡咯烷衍生物。 的式（I）化合物及其酸式盐是制备的。 在（I）中，R1 = H或低级烷基（C1-4），R2，R3 = H，低级烷基（C1-3），环烷基或-OH，n = 1或2。 的式（II）化合物与膦酰基乙酸三乙酯或溴代乙酸乙酯三苯基膦酸在强碱存在下反应，得到cpds。 具有外键双键的式（III）化合物。 在cpds。 （III），氮保护基。 与乙氧基羰基，然后酯被还原以产生酒精cpds。 这些cpds。 转化为甲磺酰基衍生物，NH（R2R3）分解。 给cpds。 （VII）。 CPDS。 （VII）水解，得到cpds。 （一世）。 CPDS。 （I）可用作制剂中的中间体。 的喹诺酮或头孢菌素抗生素。
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公开(公告)号：KR1019930007901A
公开(公告)日：1993-05-20
申请号：KR1019910018097
申请日：1991-10-15
Applicant: 한국화학연구원
IPC: C07D207/18
Abstract: 본 발명은 다음 일반식(Ⅰ)의 표시되는 아자비시클로아민 화합물과 그의 제조방법에 관한 것으로, 더욱 상세하게는, 퀼놀론 카르복실산 항균제, 세팔로스포린 항생제 또는 다른 항생물질이나 다른 의약품의 측쇄용 중간체로 유용한 불포화 아자비시클로아민 화합물과 이들 화합물의 염 및 그의 제조방법에 관한 것이다.
상기 식에서, R은 수소원자 또는 아민보호기이고, R
1 , R
2 는 서로 같거나 다른 치환기로서, 수소원자, 저급알킬기, 아실기, 치환 또는 치환되지 않은 벤조일기 또는 나프토일기, 알콕시카르보닐기, 또는 치환 또는 치환되지 않은 벤질옥시카르보닐기이고, n은 1 내지 4의 정수이다.
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